ArticleInternational journal of pharmaceutics: X2022
Preparation, characterization, and pharmacokinetics of rivaroxaban cocrystals with enhanced in vitro and in vivo properties in beagle dogs.
Article in International journal of pharmaceutics: X, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 19 citations in OpenAlex.
- In-vitro Assessment of Immediate Release Rivaroxaban Coated Fixed Dose Combination Tablets with Extended Release Molnupiravir for the Management of Coagulopathy Associated with COVID.Pharmaceutical research · 2026Article
- Enhancement of the Solubility and Dissolution Profile of Rivaroxaban by the Antisolvent Precipitation Technique: A Promising Approach.Polymers · 2026Article
- Pharmaceutical Co-Crystal Formulation of Rivaroxaban with Niacinamide: Preparation, Characterization, and In Vitro Release Evaluation.Materials (Basel, Switzerland) · 2026Article
- Novel Drug-Drug Cocrystalline Forms of Carbamazepine with Sulfacetamide: Preparation, Characterization, and In Vitro/In Vivo Performance Evaluation.Pharmaceutics · 2025Article
- Potential application of sucrose acetate isobutyrate, and glyceryl monooleate for nanonization and bioavailability enhancement of rivaroxaban tablets.Pharmaceutical science advances · 2024Article
- Development and Evaluation of Lactose-Free Single-Unit and Multiple-Unit Preparations of a BCS Class II Drug, Rivaroxaban.Pharmaceutics · 2024Article
- Solubilization techniques used for poorly water-soluble drugs.Acta pharmaceutica Sinica. B · 2024Review
- The development of an innovative method to improve the dissolution performance of rivaroxaban.Heliyon · 2024Article
- Enhancing the Stability, Solubility, and Antioxidant Activity of Cinchonine through Pharmaceutical Cocrystallization.Pharmaceutical research · 2024Article
- Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems.Pharmaceutics · 2023Review
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rivaroxaban (RIV) is a direct Factor Xa inhibitor anticoagulant, but the oral bioavailability of RIV is estimated to be only 60% due to its poor solubility. The aim of the present study was to improve the solubility and bioavailability of RIV. Five cocrystals-p-hydroxybenzoic acid (HBA), 2,4-dihydroxybenzoic acid (DBA), nicotinamide (NA), isonicotinamide (IA), and succinic acid (SA)-were used as cofomers and were successfully obtained and characterized by powder X-ray diffraction, thermal analysis, and Fourier transform infrared spectra. RIV-DBA and RIV-HBA cocrystals showed obvious improvements in solubility, dissolution (under sink conditions), and intrinsic dissolution rates versus RIV. Moreover, the dissolution of RIV-HBA, RIV-DBA, and RIV-SA cocrystals under non-sink conditions showed obvious "spring and parachute" patterns. The in vitro permeability levels in a Caco-2 cell model of RIV-DBA and RIV-IA cocrystals were significantly improved versus RIV. Pharmacokinetic studies in beagle dogs showed that RIV-DBA and RIV-HBA cocrystals had higher bioavailability than RIV. The enhancements in solubility and bioavailability indicate the potential of RIV cocrystals as a better candidate for the treatment of thrombosis versus RIV.
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